反应详情

3-(Trifluoromethyl)benzenesulfonyl chloride (3.23 g, 13.2 mmol) was added to a solution of 2-(piperidin-4-yloxy)isoindoline-1,3-dione trifluoroacetic acid (3.56 g, 9.80 mmol) and N,N-diisopropylethylamine (7.10 g, 55.0 mmol) in CH2Cl2 (85 ml), and stirred at room temperature for 17 hours. The reaction mixture was washed with aqueous 1 N HCl solution (20 ml×3), aqueous NaHCO3 solution (20 ml×3), brine (20 ml×2), dried over Na2SO4, filtered and concentrated in vacuo to give 2-(1-(3-(trifluoromethyl)phenylsulfonyl)piperidin-4-yloxy)isoindoline-1,3-dione (4.12 g, 93%) as a white solid: LCMS: 454 [M+1]+.

1. washThe reaction mixture was washed with aqueous 1 N HCl solution (20 ml×3), aqueous NaHCO3 solution (20 ml×3), brine (20 ml×2)
2. dry with materialdried over Na2SO4
3. filtrationfiltered
4. concentrationconcentrated in vacuo